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FAS inhibitor | BI 99179

Molecule

Reviews

Target protein:

FAS

Probe Name:

BI 99179

MOLECULAR WEIGHT [DA]:

391.5

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In stock:

37

Chemical structure

Highlights

The non-covalent inhibitor of type I fatty acid synthase (FAS) is a potent and selective compound suitable for in vitro and in vivo validation of FAS as a therapeutic target. The compound has significant peripheral and central exposure upon oral administration in rats.1 The optical antipode BI 99990 is offered as in vitro negative control.

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Mammalian type I fatty acid synthase (FAS) is a key enzyme for lipogenesis and highly expressed in lipogenic tissues. While most tissues, except liver and adipose tissue, have low levels of FAS expression and activity, FAS is over expressed in many cancers.2, 3

FAS inhibition could be a potential way to treat obesity.4

It has been reported that inhibitors of FAS reduce the production of sebum in sebocytes,5 suggesting topical FAS inhibition as a potential anti-acne approach.

The reported involvement of FAS in the mechanisms of viral infection and replication suggests that FAS inhibition could be applied as an antiviral principle8, 9, 10.

The optical antipode BI 99990 can be used as negative control (IC50 FAS = >3000 nM). We tested BI 99990 also in vivo to assess if the observed adverse effects for BI 99719 are rather compound or target specific with the result that the adverse effects have not been observed or have been less pronounced with BI 99990. (For more details see in vivo pharmacology section.) BI 99990 showed additional adverse effects at 50 mg/kg, therefore the compound is not suitable for further studies in rats and should be only used in vitro.